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Application of (R)- flurbiprofenester in pharmacy, injection thereof and method for preparing the same

A technology of flurbiprofen axetil and injection, applied in the field of pharmaceuticals - flurbiprofen axetil, which can solve the problems that it is difficult to make injection forms, patients cannot use it, and cannot take oral medication.

Inactive Publication Date: 2006-02-22
黄文豪
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the problem is that (R)-flurbiprofen or (S)-flurbiprofen of a single enantiomer is insoluble in water, and it is difficult to make an injection form, which makes it unusable for patients who cannot take oral medication, especially after surgery Or cancer patients are often unable to take oral medication

Method used

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  • Application of (R)- flurbiprofenester in pharmacy, injection thereof and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Mix 6 grams of 1-(acetoxy)ethyl ester (R)-flurbiprofen axetil [(R)-Flurbiprofen Axetil], 3.6 grams of lecithin, 0.15 grams of sodium oleate soap, 0.15 grams of phosphatidic acid and 30 grams of Add soybean oil into the emulsification tank, keep the temperature at 40-75°C, stir to mix and dissolve. Add 200ml of water for injection, then 7.5 grams of glycerin, add water for injection and stir to make about 300ml of coarse emulsion. Then pour the coarse emulsion into the homogenizer, and homogenize under high pressure (500kg / cm 2 ). Phosphate buffer was added, and the pH was adjusted to 5.5 with citrate. After the medicinal solution is filtered under pressure, the known injection preparation process is operated to obtain (R)-flurbiprofen axetil injection.

Embodiment 2

[0012] Mix 3 grams of 1-(acetoxy)ethyl ester (R)-flurbiprofen axetil [(R)-Flurbiprofen Axetil], 3.6 grams of lecithin, 0.15 grams of sodium oleate soap, 0.15 grams of cholesterol and 30 grams of Add soybean oil into the emulsification tank, keep the temperature at 40-75°C, stir to mix and dissolve. Add 200ml of water for injection, then 7.5 grams of glycerin, add water for injection and stir to make about 300ml of coarse emulsion. Then pour the coarse emulsion into the homogenizer, and homogenize under high pressure (500kg / cm 2 ). Phosphate buffer was added, and the pH was adjusted to 8.5 with citrate. After the medicinal solution is filtered under pressure, the known injection preparation process is operated to obtain (R)-flurbiprofen axetil injection.

Embodiment 3

[0014] 1.5 grams of 1-(acetoxy)ethyl ester (R)-flurbiprofen axetil [(R)-Flurbiprofen Axetil], 3.6 grams of lecithin, 0.15 grams of sodium oleate soap, 0.15 grams of phosphatidic acid and 30 grams Add soybean oil into the emulsification tank, keep the temperature at 40-75°C, stir to mix and dissolve. Add 200ml of water for injection, then 7.5 grams of glycerin, add water for injection and stir to make about 300ml of coarse emulsion. Then pour the coarse emulsion into the homogenizer, and homogenize under high pressure (500kg / cm 2 ). Disodium hydrogen phosphate buffer was added, and the pH was adjusted to 6.5 with citric acid. After the medicinal solution is filtered under pressure, the known injection preparation process is operated to obtain (R)-flurbiprofen axetil injection.

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Abstract

The invention relates to the use of (R)- flurbiprofenester in preparing medicament for analgesia and treatment of cancer and senile dementia, the invention also relates to a (R)-Flurbiprofen Axetil injection as main ingredient of the medicament, emulsifier of emulsibility constituents and solvent of soluble constituents. The invention also relates to the process for preparing the (R)-Flurbiprofen Axetil injection.

Description

(1) Technical field: [0001] The present invention relates to the use of (R)-flurbiprofen axetil in pharmacy, especially the use of (R)-flurbiprofen axetil in the preparation of drugs for analgesia and treatment of cancer or Alzheimer's disease; the present invention also It relates to (R)-flurbiprofen axetil injection and a preparation method thereof. (2) Background technology [0002] Flurbiprofen is a widely used non-steroidal anti-inflammatory drug (non-steroid anti-inflammatory drugs, NSAIDs), has anti-inflammatory and analgesic effects, because flurbiprofen is insoluble in water, it is difficult to make injections. Flurbiprofen Axetil (Flurbiprofen Axetil), chemical name: 2-fluoro-α-methyl-[1,1'-diphenyl]-4-acetic acid 1-(acetoxy)ethyl ester, colorless To light yellow transparent oil, it is the prodrug of flurbiprofen, has certain lipophilicity, can be dissolved in soybean oil to make lipid microspheres (Lipomicrospheres, LM) emulsion preparation, used for intravenous ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/215A61K9/107A61P1/04A61P29/00A61P35/00A61P25/28
Inventor 黄文豪
Owner 黄文豪
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